奥司他韦类似物的合成和抗贾第虫活性评估。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL Bioorganic & Medicinal Chemistry Letters Pub Date : 2024-11-20 DOI:10.1016/j.bmcl.2024.130035

Harrison W VanKoten, Breanna Pence, James R Klinkenberg, Siddhartha Das, Steven E Patterson

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引用次数: 0

摘要

我们早些时候曾报道过，抗病毒药物奥司他韦（Osm，Tamiflu®）可抑制滋养体附着在肠上皮细胞上并在培养过程中产生囊肿。Osm 还能分解脂质筏（LRs）和贾第鞭毛虫胞外囊泡（EVs）的生物生成。在目前的研究中，我们利用磷酸奥司他韦衍生合成了 41 种 Osm 类似物。这些化合物对贾第鞭毛虫的生长和包囊的产生进行了测试。结果发现，与母体奥司他韦相比，其中四种类似物，即化合物 3b、2c、11i 和 11d 对滋养体和包囊具有更强的活性。对这些制剂作用机制的研究正在进行中，将在适当的时候报告。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Synthesis and evaluation of anti-Giardia activity of oseltamivir analogs.

We reported earlier that oseltamivir (Osm, Tamiflu®), an anti-viral agent, inhibits the attachment of trophozoites to intestinal epithelial cells and cyst production in culture. Osm also disassembles lipid rafts (LRs) and the biogenesis of extracellular vesicles (EVs) by Giardia. In the current study, we synthesized forty-one Osm analogs with the derivatization of oseltamivir phosphate. These compounds were tested on giardial growth, and cyst production. Of these, four analogs, i.e., compounds 3b, 2c, 11i, and 11d, were found to have superior activities against trophozoites and cysts compared to the parent oseltamivir. Investigation of the mechanism(s) of action of these agents are in progress and will be reported in due course.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.